JP2021505551A5 - - Google Patents
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- Publication number
- JP2021505551A5 JP2021505551A5 JP2020529491A JP2020529491A JP2021505551A5 JP 2021505551 A5 JP2021505551 A5 JP 2021505551A5 JP 2020529491 A JP2020529491 A JP 2020529491A JP 2020529491 A JP2020529491 A JP 2020529491A JP 2021505551 A5 JP2021505551 A5 JP 2021505551A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- isomer
- hydrate
- solvate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 102
- 150000003839 salts Chemical class 0.000 claims description 48
- 206010028980 Neoplasm Diseases 0.000 claims description 47
- 239000012453 solvate Substances 0.000 claims description 46
- 201000011510 cancer Diseases 0.000 claims description 32
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 201000010099 disease Diseases 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 206010009944 Colon cancer Diseases 0.000 claims description 9
- 206010033128 Ovarian cancer Diseases 0.000 claims description 9
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 9
- 208000029742 colonic neoplasm Diseases 0.000 claims description 9
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims description 8
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 8
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims description 8
- 229920000642 polymer Polymers 0.000 claims description 8
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims description 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- 208000030090 Acute Disease Diseases 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 241000894006 Bacteria Species 0.000 claims description 6
- 241000233866 Fungi Species 0.000 claims description 6
- 206010025323 Lymphomas Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 230000001154 acute effect Effects 0.000 claims description 6
- 210000000941 bile Anatomy 0.000 claims description 6
- 208000037976 chronic inflammation Diseases 0.000 claims description 6
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 6
- 244000005700 microbiome Species 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- -1 vinylcarbonyl group Chemical group 0.000 claims description 6
- 230000003612 virological effect Effects 0.000 claims description 6
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims description 5
- 102000009027 Albumins Human genes 0.000 claims description 4
- 108010088751 Albumins Proteins 0.000 claims description 4
- 239000004471 Glycine Substances 0.000 claims description 4
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims description 4
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 4
- YPIGGYHFMKJNKV-UHFFFAOYSA-N N-ethylglycine Chemical compound CC[NH2+]CC([O-])=O YPIGGYHFMKJNKV-UHFFFAOYSA-N 0.000 claims description 4
- 108010065338 N-ethylglycine Proteins 0.000 claims description 4
- VDIPNVCWMXZNFY-UHFFFAOYSA-N N-methyl-beta-alanine Chemical compound CNCCC(O)=O VDIPNVCWMXZNFY-UHFFFAOYSA-N 0.000 claims description 4
- 108010077895 Sarcosine Proteins 0.000 claims description 4
- 239000012190 activator Substances 0.000 claims description 4
- 235000004279 alanine Nutrition 0.000 claims description 4
- 235000001014 amino acid Nutrition 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 229940000635 beta-alanine Drugs 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 230000003013 cytotoxicity Effects 0.000 claims description 4
- 231100000135 cytotoxicity Toxicity 0.000 claims description 4
- GCHPUFAZSONQIV-UHFFFAOYSA-N isovaline Chemical compound CCC(C)(N)C(O)=O GCHPUFAZSONQIV-UHFFFAOYSA-N 0.000 claims description 4
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims description 4
- 229940043230 sarcosine Drugs 0.000 claims description 4
- 206010000830 Acute leukaemia Diseases 0.000 claims description 3
- 206010061424 Anal cancer Diseases 0.000 claims description 3
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 3
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims description 3
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 206010005949 Bone cancer Diseases 0.000 claims description 3
- 208000018084 Bone neoplasm Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 3
- 208000009738 Connective Tissue Neoplasms Diseases 0.000 claims description 3
- 208000009129 Ear Neoplasms Diseases 0.000 claims description 3
- 206010014733 Endometrial cancer Diseases 0.000 claims description 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 3
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims description 3
- 208000032612 Glial tumor Diseases 0.000 claims description 3
- 206010018338 Glioma Diseases 0.000 claims description 3
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 3
- 208000017604 Hodgkin disease Diseases 0.000 claims description 3
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010051696 Metastases to meninges Diseases 0.000 claims description 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 3
- 201000010133 Oligodendroglioma Diseases 0.000 claims description 3
- 208000002471 Penile Neoplasms Diseases 0.000 claims description 3
- 206010034299 Penile cancer Diseases 0.000 claims description 3
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims description 3
- 206010034811 Pharyngeal cancer Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 3
- 206010038389 Renal cancer Diseases 0.000 claims description 3
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 3
- 206010039491 Sarcoma Diseases 0.000 claims description 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 3
- 206010057644 Testis cancer Diseases 0.000 claims description 3
- 206010062129 Tongue neoplasm Diseases 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 208000006593 Urologic Neoplasms Diseases 0.000 claims description 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
- 208000014070 Vestibular schwannoma Diseases 0.000 claims description 3
- 208000004064 acoustic neuroma Diseases 0.000 claims description 3
- 208000009956 adenocarcinoma Diseases 0.000 claims description 3
- 239000003708 ampul Substances 0.000 claims description 3
- 201000011165 anus cancer Diseases 0.000 claims description 3
- 201000000053 blastoma Diseases 0.000 claims description 3
- 210000004027 cell Anatomy 0.000 claims description 3
- 201000010881 cervical cancer Diseases 0.000 claims description 3
- 201000008184 embryoma Diseases 0.000 claims description 3
- 210000003238 esophagus Anatomy 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 201000009277 hairy cell leukemia Diseases 0.000 claims description 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 3
- 201000002313 intestinal cancer Diseases 0.000 claims description 3
- 201000010982 kidney cancer Diseases 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 201000007270 liver cancer Diseases 0.000 claims description 3
- 208000014018 liver neoplasm Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 3
- 230000002188 osteogenic effect Effects 0.000 claims description 3
- 230000000010 osteolytic effect Effects 0.000 claims description 3
- 201000008968 osteosarcoma Diseases 0.000 claims description 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 3
- 229940127557 pharmaceutical product Drugs 0.000 claims description 3
- 208000023974 pharynx neoplasm Diseases 0.000 claims description 3
- 206010038038 rectal cancer Diseases 0.000 claims description 3
- 201000001275 rectum cancer Diseases 0.000 claims description 3
- 201000000849 skin cancer Diseases 0.000 claims description 3
- 210000004500 stellate cell Anatomy 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 208000011580 syndromic disease Diseases 0.000 claims description 3
- 201000003120 testicular cancer Diseases 0.000 claims description 3
- 201000006134 tongue cancer Diseases 0.000 claims description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- 206010046766 uterine cancer Diseases 0.000 claims description 3
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims description 2
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims description 2
- 125000004069 aziridinyl group Chemical group 0.000 claims description 2
- 125000002228 disulfide group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000004185 ester group Chemical group 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- 150000002500 ions Chemical class 0.000 claims description 2
- ZBKFYXZXZJPWNQ-UHFFFAOYSA-N isothiocyanate group Chemical group [N-]=C=S ZBKFYXZXZJPWNQ-UHFFFAOYSA-N 0.000 claims description 2
- 239000002502 liposome Substances 0.000 claims description 2
- 239000002207 metabolite Substances 0.000 claims description 2
- 239000002105 nanoparticle Substances 0.000 claims description 2
- 229920005615 natural polymer Polymers 0.000 claims description 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 2
- 125000005030 pyridylthio group Chemical group N1=C(C=CC=C1)S* 0.000 claims description 2
- 125000006850 spacer group Chemical group 0.000 claims description 2
- 229920001059 synthetic polymer Polymers 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims 3
- 239000000178 monomer Substances 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 8
- 0 CCNc1ccc(C)c(N)c1C(**=C)=O Chemical compound CCNc1ccc(C)c(N)c1C(**=C)=O 0.000 description 3
- 239000003814 drug Substances 0.000 description 2
- 125000003396 thiol group Chemical group [H]S* 0.000 description 2
- OLLZXQIFCRIRMH-UHFFFAOYSA-N CCCC(NC)=O Chemical compound CCCC(NC)=O OLLZXQIFCRIRMH-UHFFFAOYSA-N 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023151472A JP2023164604A (ja) | 2017-11-30 | 2023-09-19 | メイタンシノイド系薬物送達システム |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762593184P | 2017-11-30 | 2017-11-30 | |
| US62/593,184 | 2017-11-30 | ||
| PCT/US2018/063380 WO2019108975A1 (en) | 2017-11-30 | 2018-11-30 | Maytansinoid-based drug delivery systems |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023151472A Division JP2023164604A (ja) | 2017-11-30 | 2023-09-19 | メイタンシノイド系薬物送達システム |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021505551A JP2021505551A (ja) | 2021-02-18 |
| JP2021505551A5 true JP2021505551A5 (de) | 2022-01-11 |
| JPWO2019108975A5 JPWO2019108975A5 (de) | 2023-05-15 |
| JP7442821B2 JP7442821B2 (ja) | 2024-03-05 |
Family
ID=64744962
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020529491A Active JP7442821B2 (ja) | 2017-11-30 | 2018-11-30 | メイタンシノイド系薬物送達システム |
| JP2023151472A Pending JP2023164604A (ja) | 2017-11-30 | 2023-09-19 | メイタンシノイド系薬物送達システム |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023151472A Pending JP2023164604A (ja) | 2017-11-30 | 2023-09-19 | メイタンシノイド系薬物送達システム |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11572373B2 (de) |
| EP (1) | EP3717018A1 (de) |
| JP (2) | JP7442821B2 (de) |
| KR (1) | KR20200117988A (de) |
| CN (1) | CN111712263A (de) |
| AU (1) | AU2018375788A1 (de) |
| BR (1) | BR112020010989A2 (de) |
| CA (1) | CA3083985A1 (de) |
| IL (2) | IL305268A (de) |
| MX (1) | MX2020005472A (de) |
| WO (1) | WO2019108975A1 (de) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107922457B (zh) | 2015-06-19 | 2022-05-13 | 森托瑞恩生物制药公司 | 用于控制药物释放的递送系统 |
| EP3717503B1 (de) | 2017-11-30 | 2023-11-08 | LadRx Corporation | Albuminbindende prodrugs von auristatin-e-derivaten |
| CN113952464A (zh) | 2018-03-06 | 2022-01-21 | 江苏吉贝尔药业股份有限公司 | 含酮羰基的疏水性抗肿瘤药物及其应用 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4125704A (en) | 1977-09-14 | 1978-11-14 | Sri International | Phenyl-substituted rubidazone analogs |
| GB8308235D0 (en) | 1983-03-25 | 1983-05-05 | Celltech Ltd | Polypeptides |
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| GB8422238D0 (en) | 1984-09-03 | 1984-10-10 | Neuberger M S | Chimeric proteins |
| US4699880A (en) | 1984-09-25 | 1987-10-13 | Immunomedics, Inc. | Method of producing monoclonal anti-idiotype antibody |
| GB8607679D0 (en) | 1986-03-27 | 1986-04-30 | Winter G P | Recombinant dna product |
| US5225539A (en) | 1986-03-27 | 1993-07-06 | Medical Research Council | Recombinant altered antibodies and methods of making altered antibodies |
| US4946778A (en) | 1987-09-21 | 1990-08-07 | Genex Corporation | Single polypeptide chain binding molecules |
| ATE243754T1 (de) | 1987-05-21 | 2003-07-15 | Micromet Ag | Multifunktionelle proteine mit vorbestimmter zielsetzung |
| US4966999A (en) | 1988-06-07 | 1990-10-30 | Cytogen Corporation | Radiohalogenated compounds for site specific labeling |
| IL162181A (en) | 1988-12-28 | 2006-04-10 | Pdl Biopharma Inc | A method of producing humanized immunoglubulin, and polynucleotides encoding the same |
| DE69233482T2 (de) | 1991-05-17 | 2006-01-12 | Merck & Co., Inc. | Verfahren zur Verminderung der Immunogenität der variablen Antikörperdomänen |
| EP0605522B1 (de) | 1991-09-23 | 1999-06-23 | Medical Research Council | Methoden zur Herstellung humanisierter Antikörper |
| DE614989T1 (de) | 1993-02-17 | 1995-09-28 | Morphosys Proteinoptimierung | Verfahren für in vivo Selektion von Ligandenbindende Proteine. |
| DE19926154A1 (de) * | 1999-06-09 | 2000-12-14 | Ktb Tumorforschungs Gmbh | Verfahren zur Herstellung einer injizierbaren Arzneimittelzubereitung |
| GB0004297D0 (en) | 2000-02-23 | 2000-04-12 | Ucb Sa | 2-oxo-1 pyrrolidine derivatives process for preparing them and their uses |
| US6884869B2 (en) | 2001-04-30 | 2005-04-26 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| NZ547370A (en) | 2003-12-04 | 2010-09-30 | Amr Technology Inc | Vinca derivatives |
| JP5634862B2 (ja) | 2007-05-16 | 2014-12-03 | カーテーベー トゥモーアフォルシュングス ゲゼルシャフト ミット ベシュレンクテル ハフツング | 低粘度アントラサイクリン製剤 |
| EP2289558A1 (de) | 2009-08-25 | 2011-03-02 | KTB Tumorforschungsgesellschaft mbH | Bisphosphonat-Prodrugs |
| WO2012145112A2 (en) * | 2011-04-18 | 2012-10-26 | Immunogen, Inc. | Novel maytansinoid derivatives with sulfoxide linker |
| EP3327027B9 (de) | 2011-11-17 | 2021-07-07 | Pfizer Inc. | Zytotoxische peptide und antikörperwirkstoffkonjugate dafür |
| EP2630971B8 (de) | 2012-02-21 | 2017-12-13 | Vergell Medical S.A. | Kombinationen aus Arzneimittelabgabesystemen auf Albuminbasis |
| ES2701076T3 (es) * | 2012-11-24 | 2019-02-20 | Hangzhou Dac Biotech Co Ltd | Enlazadores hidrofílicos y sus usos para la conjugación de fármacos a las moléculas que se unen a las células |
| CN104650113A (zh) | 2012-12-21 | 2015-05-27 | 百奥泰生物科技(广州)有限公司 | 类美登素衍生物及其制备方法和用途 |
| US20140221429A1 (en) | 2013-02-04 | 2014-08-07 | Saud Ibrahim Al-Resayes | Heterocyclic schiff's bases as novel and new antiglycation agents |
| US9999680B2 (en) * | 2013-02-28 | 2018-06-19 | Immunogen, Inc. | Conjugates comprising cell-binding agents and maytansinoids as cytotoxic agents |
| EP3273998B1 (de) * | 2015-03-27 | 2019-09-04 | Regeneron Pharmaceuticals, Inc. | Maytansinoidderivate, konjugate davon und verfahren zur verwendung |
| US9914952B2 (en) | 2015-06-15 | 2018-03-13 | Abbott Diabetes Care, Inc. | Stabilized lactate responsive enzymes, electrodes and sensors, and methods for making and using the same |
| CN107922457B (zh) * | 2015-06-19 | 2022-05-13 | 森托瑞恩生物制药公司 | 用于控制药物释放的递送系统 |
| EP3717503B1 (de) | 2017-11-30 | 2023-11-08 | LadRx Corporation | Albuminbindende prodrugs von auristatin-e-derivaten |
-
2018
- 2018-11-30 IL IL305268A patent/IL305268A/en unknown
- 2018-11-30 JP JP2020529491A patent/JP7442821B2/ja active Active
- 2018-11-30 MX MX2020005472A patent/MX2020005472A/es unknown
- 2018-11-30 KR KR1020207018379A patent/KR20200117988A/ko not_active Application Discontinuation
- 2018-11-30 CA CA3083985A patent/CA3083985A1/en active Pending
- 2018-11-30 BR BR112020010989-4A patent/BR112020010989A2/pt unknown
- 2018-11-30 EP EP18822213.7A patent/EP3717018A1/de active Pending
- 2018-11-30 US US16/768,418 patent/US11572373B2/en active Active
- 2018-11-30 AU AU2018375788A patent/AU2018375788A1/en active Pending
- 2018-11-30 WO PCT/US2018/063380 patent/WO2019108975A1/en unknown
- 2018-11-30 CN CN201880088076.0A patent/CN111712263A/zh active Pending
- 2018-11-30 IL IL274920A patent/IL274920B2/en unknown
-
2022
- 2022-12-21 US US18/086,076 patent/US20230391794A1/en active Pending
-
2023
- 2023-09-19 JP JP2023151472A patent/JP2023164604A/ja active Pending
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